Kinase 2018:
towards new frontiers

8th RSC / SCI symposium on kinase inhibitor design

 

Monday-Tuesday, 14th-15th May 2018

Babraham Research Campus, Cambridge, UK

 

 

Registration is closed

 

Downloads and Links

Second announcement

First announcement

 

Coach travel bookings

Venue website

Venue location map

Venue site plan - Cambridge Building in centre

 

Travelodge Fourwentways online booking

Accommodation suggestions

RSC website

SCI website

 

Synopsis

With more than 25 FDA-approved small molecules, the field of kinase inhibition continues to attract significant investment from the drug discovery and development community. The 8th RSC/SCI symposium on kinases encompassed case studies of ongoing programmes as well as successful past programmes. A range of topics including CNS kinase inhibitors, allosteric inhibitors and non-oral delivery methods were covered, along with views and perspectives on the future of kinase inhibitor research.

 

Programme   Where text is highlighted thus, you may download the presentation as a .pdf

 

Monday, 14th May
09:00Registration and refreshments
10:00

Opening remarks

Martin Swarbrick, Cancer Research UK

 Session chair:  Martin Swarbrick, Cancer Research UK
10:05Keynote presentation

Targeting PI3Ks in immunity, infection and cancer

Klaus Okkenhaug, University of Cambridge and Babraham Institute, UK

10:45

Discovery and development of a novel, immunosuppressive class of lipid kinase inhibitors able to prolong allogeneic organ engraftment

James Reuberson, UCB, UK

11:20Refreshments, exhibition and posters
 

 

Session chair:  Andrew Thomas, AstraZeneca

11:50

Discovery of GDC-0077, a highly isoform selective inhibitor of PI3Kα that promotes selective degradation of mutant-p110α

Emily Hanan, Genentech, USA

12:25

Roger Griffin Memorial Lecture

Inhibitors of the mitotic kinase MPS1:  discovery of an orally bioavailable preclinical development candidate

Julian Blagg, Institute of Cancer Research, UK

13:05Lunch, exhibition and posters
 

 

Session chair:  Mihiro Sunose, Sygnature Discovery

14:05

A potent and orally bioavailable ERK1/2 series identified through fragment screening which modulates the phosphorylation and catalytic activity of ERK1/2

Valerio Berdini, Astex Pharmaceuticals, UK

14:40

NVP‐LXS196, a novel PKC inhibitor for the treatment of uveal melanoma

Julien Papillon, Novartis Institutes for Biomedical Research, USA

15:15Target residence time-guided optimization on TTK kinase results in inhibitors with potent anti-proliferative activity
Guido Zaman, Netherlands Translational Research Center, The Netherlands
15:40Refreshments, exhibition and posters
 

 

Session chair:  Pascal Savy, Charles River

16:10

Identification of low clearance indole acid AMPK activators for the treatment of diabetic nephropathy

David Ebner, Pfizer, USA

16:45

New leads from old drugs: repurposing kinase inhibitor chemotypes for tropical diseases

Michael Pollastri, Northeastern University, USA

  

Flash poster presentations - Session 1

17:20

Discovery of CDK12 inhibition as a potential new treatment for myotonic dystrophy
Nicholas Bennett, School of Life Science & School of Chemistry, University of Nottingham  P04)

17:22

The synthesis and physiochemical properties of nitrogen containing 6,5-bicyclic heterocycles
Brett Cosgrove, GlaxoSmithKline (P06)

17:24

Quantitative irreversible tethering (qIT) for covalent ligand discovery
Gregory Craven, Imperial College London (P07)

17:26

Optimisation of permeability in a series of pyrrolotriazine inhibitors of IRAK4 for the treatment of mutant MYD88L265P diffuse large B-cell lymphoma
Sébastien Degorce, IMED Biotech Unit, AstraZeneca (P08)

17:28

Dynamic equilibrium of the Aurora-A kinase activation loop revealed by single-molecule spectroscopy
Charlotte Dodson, National Heart & Lung Institute, Imperial College London (P09)

17:30

Understanding kinase potency SAR by MMPA based network analysis
Ed Griffen, MedChemica Ltd (P11)

17:32

Making the most of public domain data with Knime®: ligand-based design of selective DYRK1 inhibitors
Scott Henderson, Sussex Drug Discovery Centre, University of Sussex (P12)

17:35

Network reception, exhibition and posters

19:00Conference dinner

 

Tuesday, 15th May

 Session chair:  Martin Swarbrick, Cancer Research UK

09:00

Keynote presentation

Strategy and tactics for the discovery of Kinase inhibitors for CNS targets. A Lundbeck perspective

Klaus Bæk Simonsen, Lundbeck

09:40

Building on the success of Osimertinib - achieving CNS exposure in oncology drug discovery

Nicola Colclough, AstraZeneca, UK

10:15Refreshments, exhibition and posters
 

 

Session chair:  John Cumming, Roche

10:45

Chemical strategies for activating PINK1, a protein kinase mutated in Parkinson’s disease

Youcef Mehellou, Cardiff School of Pharmacy and Pharmaceutical Sciences, UK

11:20

BBB penetrating tetracyclic TRK-selective inhibitor CH7057288: additional efficacy against brain metastasis in vivo model

Toshiya Ito, Chugai, Japan

11:55Interactive session
  

Flash poster presentations - Session 2

12:25

Exploration of REadily AccesibLe (REAL) arrays for hit finding: identification of potent Aurora A kinase inhibitors and follow-up studies
Tatiana Matviyuk, Enamine Ltd (P14)

12:27

The design and synthesis of novel inhibitor tools of PRK2 for validation of a synthetic lethal strategy to target cancer
Fiona Scott, Sussex Drug Discovery Centre, University of Sussex (P18)

12:29

Deciphering kinase SAR using electrostatics
Martin Slater, Cresset (P19)

12:31

Send cancer PAK-ing: optimisation of novel p-21 activated kinase inhibitors
Geoffrey Smith, Cancer Research UK Therapeutic Discovery Laboratories (P20)

12:33

Design and synthesis of Janus kinase inhibitors for inhaled delivery and the importance of aldehyde oxidase metabolism in the lung
Christopher Wellaway, GlaxoSmithKline (P23)

12:35

MPL-7097, an ESMTM p38 MAPK inhibitor
Natalie Winfield, Domainex Ltd (P24)

12:40

Lunch, exhibition and posters

 

13:35

 

Poster prize-giving

 

 

Session chair:  Andrew Thomas, AstraZeneca

13:40Quantitative, wide-spectrum kinase target engagement profiling in live cells
Craig Malcolm, Promega UK Ltd, UK
14:05

Discovery of AZD1390: a brain penetrant ATM kinase inhibitor

Thomas Hunt, AstraZeneca, UK

14:40

Keynote presentation

Structural mechanisms of regulation of the PI3Ks and related kinases

Roger Williams, MRC Laboratory of Molecular Biology, UK

15:20

Closing remarks

Andrew Thomas, AstraZeneca

15:25

Close

 

Who should attend?
This event was aimed at all scientists interested in furthering their knowledge of kinases. It also had wider appeal to members of the drug discovery community eager to understand how enzyme inhibitor programmes are approached and executed across the pharmaceutical industry.

 

Call for Posters

A poster session took place at the end of Day 1. The closing date for one-page abstract submissions was 31st March 2018. When submitting posters, delegates were asked to indicate whether they were prepared to give a single-slide summary of their poster in a formal presentation session.

 

Registration, Fees and Bursaries

Registration fees include Monday evening's dinner and free coach transport between Travelodge Fourwentways and Whittlesford Parkway railway station (one coach for each trip).

Early rates for payments received by 7th February
£269  RSC or SCI member
£325  Non-member
£140  RSC or SCI student* member
£159  Student* non-member

Standard rates for payments received between 8th February and 11th April
£324  RSC or SCI member
£392  Non-member
£168  RSC or SCI student* member
£196  Student* non-member

Late rates for payments received from 12th April onwards
£40  Late payment fee to be added to the above standard rates

* Student is undergraduate or post-graduate, not post-doc, and does not apply to students in paid employment.
Member is paid-up member of the RSC or SCI.

Some student bursaries were available, and the closing date was 2nd April. 

 

Cancellation Policy

In the event of cancellation by 29th April 2018, 80% of the fee paid will be refunded. Cancellations must be received in writing. Refunds will not be possible after that date although substitutions are possible at any time. In the unlikely event of cancellation of the meeting, fees paid will be refunded in full.
 

Exhibition

There was a relevant trade exhibition and the charge is £952.  This rate included:

- stand space measuring 3 m wide x 2 m deep

- table measuring 1.5 m wide x 0.75 m deep x 0.73 m high

- access to electricity and wi-fi

- inclusion of a promotional slide to be played on rotation on the main screen during breaks
- logo acknowledgement in the delegate handbook

- one full delegate with all catering.

 

Delegate pack inserts were booked at £250 - no more than two sheets of A4 fixed together.

 

Sponsorship

We are grateful to our sponsors for their kind support of the event.

 

 

We are grateful to EFMC and COMS for supporting this event

 

Venue

Babraham Research Campus, Babraham Hall, Babraham, Cambridge, CB22 3AT UK.  There is ample free parking on site, and no parking permits are required.

 

Venue location map

Venue location weblink

 

Accommodation

A number of bedrooms were held (via InCorporate Venues) at the Travelodge Fourwentways, and rooms were available to book online.  Any unbooked bedrooms were released at midday on 16th March, and cancellation is not possible thereafter.

 

Free coach transport (see below) was provided between the venue and the Travelodge Fourwentways and Whittlesford Parkway railway station.    Other hotel suggestions may be found here.

 

Coach Transport

A coach was booked to provide transport as outlined below.   This was provided gratis, and you were advised to book your requirements at the time of registration, as the limited number of spaces were allocated on a "first come, first served" basis.   Timings are inserted below.

 

Please review this listing to check your bookings are correct.

 

Monday, 14th May - morning
08:40   Whittlesford Parkway railway station
08:50   Travelodge Cambridge Fourwentways
08:50   Babraham Research Campus

Monday, 14th May - evening
21:00   Babraham Research Campus
21:10   Travelodge Cambridge Fourwentways -
fully booked
21:20   Whittlesford Parkway railway station -
fully booked

Tuesday, 15th May - morning
08:25   Whittlesford Parkway railway station
08:35   Travelodge Cambridge Fourwentways
08:45   Babraham Research Campus

Tuesday, 15th May – afternoon
15:25    Babraham Research Campus
15:45    Whittlesford Parkway railway station
 

Organising Committee

John CummingRoche and SCI
John HarrisCJH Consultants
Pascal SavyCharles River and SCI
Mihiro SunoseSygnature and RSC

Martin Swarbrick

(chair)

Cancer Research UK and RSC
Andrew ThomasAstraZeneca

     

Secretariat Contact

Maggi Churchouse Events, 3 East Barn, Market Weston Road, Thelnetham, Diss IP22 1JJ, UK

E-mail Maggi Churchouse

Telephone: +44 (0)1359 221004

 

Registration is closed